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Cubebin and derivatives as inhibitors of mitochondrial complex I. Proposed interaction with subunit B8.
Saraiva, Juliana; Siqueira, Claudia Meirelles; de Paula da Silva, Carlos Henrique Tomich; Barreto da Silva, Vinicius; Tudella, Valeria Gomes; Silva, Rosangela; Andrade E Silva, Marcio Luis; Dorta, Daniel Junqueira; Bastos, Jairo Kenupp; Uyemura, Sergio Akira; de Albuquerque, Sergio; Curti, Carlos.
Afiliação
  • Saraiva J; Departamento de Analises Clinicas, Toxicologicas e Bromatologicas, Faculdade de Ciencias Farmaceuticas de Ribeirao Preto, Universidade de Sao Paulo, Ribeirao Preto, SP, Brazil.
J Enzyme Inhib Med Chem ; 24(2): 599-606, 2009 Apr.
Article em En | MEDLINE | ID: mdl-18825534
ABSTRACT
The effects on mitochondrial respiration and complex I NADH oxidase activity of cubebin and derivatives were evaluated. The compounds inhibited the state 3 glutamate/malate-supported respiration of hamster liver mitochondria with IC(50) values ranging from 12.16 to 83.96 microM. NADH oxidase reaction was evaluated in submitochondrial particles. The compounds also inhibited this activity, showing the same order of potency observed for effects on state 3 respiration, as well as a tendency towards a non-competitive type of inhibition (K(I) values ranging from 0.62 to 16.1 microM). A potential binding mode of these compounds with complex I subunit B8, assessed by docking calculations, is proposed.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Lignanas / Complexo I de Transporte de Elétrons Limite: Animals Idioma: En Ano de publicação: 2009 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Lignanas / Complexo I de Transporte de Elétrons Limite: Animals Idioma: En Ano de publicação: 2009 Tipo de documento: Article